Chem Basis PPIs 9

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  1. Electron donating groups on benzimidazole increase the ¬¬¬¬¬¬¬¬¬¬¬¬¬__________ which increases ___________.
    percent of ionized N3, which increases the d+ of C2
  2. Doe the e- donating groups increase the reactivity of the pyridine nucleophile or the benzimidazole electrophile?
    Both
  3. E- donating groups increase the reactivity of the pyridine nucleophile or the benzimidazole electrophile, ehcih has what effect on the speed of PPI activation?
    Increases
  4. (True/False) Electron donating groups make the pyridine N1 a better nucleophile and the benzimidazole C2 a better electrophile.
    True
  5. Of the three possible cationic forms of the PPI at the canniculus pH, which is the essential form for conducting the PPI activation reaction?
    Protonated Benzimidazole-Free Pyridine (monocation)
  6. _______ cationic forms of the proton pump inhibitor are possible in the very low pH of the canniculus.
    Three
  7. Why does it take 4 - 5 days for gastric pH to return to normal after PPI use?
    Because of the fairly irreversible inhibition of the pump by the PPI
  8. What is the onset of action for PPIs?
    3 – 5 days
  9. Which PPI is not metabolized by CYP enzymes?
    Rabeprazole
  10. Which CYP enzyme is most involved in inactivation of the various PPI structures?
    CYP2C19
  11. What CYP enzyme do most PPIs inhibit?
    CYP2C19
  12. Which PPIs inhibit CYP2C19 most effectively?
    Omeprazole and esomeprazole
  13. Which CYP often metabolizes PPIs, but not as much as CYP2C19?
    CYP3A4
  14. Which CYP enzyme is responsible for the oxidation of the PPI sulfinyl to inactive sulfone?
    CYP3A4
  15. Which CYP enzyme is usually a second string enzymatic player in hydroxylations?
    CYP3A4
  16. Which CYP enzyme is responsible for O-dealkylation of PPIs?
    CYP2C19
  17. Which CYP enzyme is responsible for Benzylic hydroxylation of PPIs?
    CYP2C19
  18. Which CYP enzyme is responsible for Aromatic hydroxylation of PPIs?
    CYP2C19
  19. Poor PPI 2C19 metabolizer phenotypes get more or less drug action per dose with few DDI risks?
    More
  20. Extensive 2C19 metabolizer phenotypes may or may not respond well to CYP2C19-dependent PPIs?
    May not
  21. What non-CYP mediated reaction occurs with Rabeprazole?
    Cystolic oxidation
  22. What non-CYP mediated reaction occurs with pantoprazole?
    Phase II sulfate conjugation
  23. What non-CYP mediated reaction occurs with all PPIs?
    Reduction of sulfinyl
Author:
kyleannkelsey
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251730
Card Set:
Chem Basis PPIs 9
Updated:
2013-12-08 21:46:43
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Chem Basis PPIs 9
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